The present invention describes the preparation and respective application of innovative non-nitrocatechol COMT inhibitors, that manifested improved pharmacokinetic and pharmacodynamic properties compared to those currently used in the clinic (e.g. tolcapone, entacapone, opicapone).
COMT has been an interesting pharmacological target for adjuvant terapy on Parkison´s disease and other CNS disorders. However, current COMT inhibitors on the therapeutic are associated with problems related to their ADMET properties, namely short half-lives, citotoxicity, and low BBB permeability.
Selective COMT inhibitors; Suitable lipophilicity for BBB permeability; Less cytotoxic than standard COMT inhibitors.
Co-adjuvant drugs for treatment of Parkinson´s disease; Therapeutic agents for other neuropsychiatric disorders associated with low dopamine levels.
